Hydrochloric Acid → (R)-2-amino-1-(3-but-2-ynyloxy-3-o-tolyl-azetidin-1-yl)-3-(4-methoxyphenyl)propan-1-one

HRID 540433노트

반응식

HRID 540433 반응식
C(OC(=O)[NH:7][C@H:8]([CH2:27][C:28]1[CH:33]=[CH:32][C:31]([O:34][CH3:35])=[CH:30][CH:29]=1)[C:9]([N:11]1[CH2:14][C:13]([O:22][CH2:23][C:24]#[C:25][CH3:26])([C:15]2[CH:20]=[CH:19][CH:18]=[CH:17][C:16]=2[CH3:21])[CH2:12]1)=[O:10])(C)(C)C.Cl>C(OCC)(=O)C>[NH2:7][C@H:8]([CH2:27][C:28]1[CH:29]=[CH:30][C:31]([O:34][CH3:35])=[CH:32][CH:33]=1)[C:9]([N:11]1[CH2:12][C:13]([O:22][CH2:23][C:24]#[C:25][CH3:26])([C:15]2[CH:20]=[CH:19][CH:18]=[CH:17][C:16]=2[CH3:21])[CH2:14]1)=[O:10]

참가 물질

4

반응물 2

HCID 313Hydrochloric AcidHCID 67295764tert-butyl[(R)-2-(3-but-2-ynyloxy-3-o-tolylazetidin-1-yl)-1-(4-methoxybenzyl)-2-oxo-ethyl]carbamate

생성물 1

HCID 66988366(R)-2-amino-1-(3-but-2-ynyloxy-3-o-tolyl-azetidin-1-yl)-3-(4-methoxyphenyl)propan-1-one수율 116.5%

시약·촉매·용매 1

HCID 8857Ethyl Acetate용매

실험 절차

1.7 g (3.5 mmol) of tert-butyl[(R)-2-(3-but-2-ynyloxy-3-o-tolylazetidin-1-yl)-1-(4-methoxybenzyl)-2-oxo-ethyl]carbamate are solubilised in 45 ml (135 mmol) of a 3M solution of hydrochloric acid in ethyl acetate. After stirring for 3 h at ambient temperature, the mixture is concentrated. 1.6 g of (R)-2-amino-1-(3-but-2-ynyloxy-3-o-tolylazetidin-1-yl)-3-(4-methoxyphenyl)-propan-1-one are obtained in the form of a beige solid with a quantitative yield.

후처리

  1. concentrationthe mixture is concentrated

출처 및 근거

ORD 기록
ord-8c6b4f87d9334b44a5f9a0cdf70a3259
출처 데이터셋
uspto-grants-2014_10
특허 번호
US08871187B2

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